Cefuroxime; Indications/Uses, Dosage, Side Effects, Interactions

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Cefuroxime is a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefuroxime interferes with an autolysin inhibitor. This effect is bactericidal.

Mechanism of Action of Cefuroxime

Cefuroxime, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefuroxime interferes with an autolysin inhibitor.

Cefuroxime, a beta-lactam antibiotic similar to penicillins, inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) that are located inside the bacterial cell wall. Penicillin-binding proteins are responsible for several steps in the synthesis of the cell wall and are found in quantities of several hundred to several thousand molecules per bacterial cell. Penicillin-binding proteins vary among different bacterial species. Thus, the intrinsic activity of cefuroxime, as well as the other cephalosporins and penicillins against a particular organism, depends on their ability to gain access to and bind with the necessary PBP. Like all beta-lactam antibiotics, cefuroxime’s ability to interfere with PBP-mediated cell wall synthesis ultimately leads to cell lysis. Lysis is mediated by bacterial cell wall autolytic enzymes (i.e., autolysins). The relationship between PBPs and autolysins is unclear, but it is possible that the beta-lactam antibiotic interferes with an autolysin inhibitor. Cefuroxime possesses activity against both Gram-positive and Gram-negative bacteria. The drug retains antibacterial activity in the presence of certain beta-lactamases, both penicillinase, and cephalosporins; however hydrolysis by other beta-lactamases, alteration of the PBP, and decreases permeability results in resistance to cefuroxime.

Indications of Cefuroxime

For the treatment of many different types of bacterial infections such as bronchitis, sinusitis, tonsillitis, ear infections, skin infections, gonorrhea, and urinary tract infections.

  • Acute bacterial exacerbation of chronic bronchitis
  • Bacterial infections
  • Bloodstream infections
  • Bone and joint infections
  • Gonorrhea
  • Impetigo
  • Pneumonia
  • Urinary tract infection
  • Skin or soft tissue infection
  • Skin and structure infection
  • Septicemia
  • Meningitis
  • Joint infection
  • Osteomyelitis
  • Surgical prophylaxis
  • Tonsillitis/pharyngitis
  • Sinusitis
  • Intra abdominal infection
  • Appendicitis
  • Wound infection
  • Lower respiratory tract infection maxillary sinusitis
  • Otitis media bacterial
  • Skin and subcutaneous tissue bacterial infections
  • Pharyngitis
  • Bladder infection
  • Epiglottitis
  • Kidney infections
  • Otitis media
  • Peritonitis
  • Sepsis
  • Skin and structure /soft tissue  infection

Cefuroxime is usually active against the following microorganisms in vitro.

Commonly susceptible species
Gram-positive aerobes:

Staphylococcus aureus (methicillin-susceptible)*

Coagulase negative staphylococcus (methicillin susceptible)

Streptococcus pyogenes

Streptococcus agalactiae

Gram-negative aerobes:

Haemophilus influenzae

Haemophilus parainfluenzae

Moraxella catarrhalis

Spirochaetes:

Borrelia burgdorferi

Microorganisms for which acquired resistance may be a problem
Gram-positive aerobes:

Streptococcus pneumoniae

Gram-negative aerobes:

Citrobacter freundii

Enterobacter aerogenes

Enterobacter cloacae

Escherichia coli

Klebsiella pneumoniae

Proteus mirabilis

Proteus spp. (other than P. vulgaris)

Providencia spp.

Gram-positive anaerobes:
Peptostreptococcus spp.

Propionibacterium spp.

Gram-negative anaerobes:

Fusobacterium spp.

Bacteroides spp.

Inherently resistant microorganisms
Gram-positive aerobes:

Enterococcus faecalis

Enterococcus faecium

Gram-negative aerobes:

Acinetobacter spp.

Campylobacter spp.

Morganella morganii

Proteus vulgaris

Pseudomonas aeruginosa

Serratia marcescens

Gram-negative anaerobes:

Bacteroides fragilis

Others:

Chlamydia spp.

Mycoplasma spp.

Legionella spp.

* All methicillin-resistant S. aureus are resistant to cefuroxime.

Contra-Indications of Cefuroxime

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams, and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • Allergies cephalosporins & beta-lactams

Dosage of Cefuroxime

Strengths: 125 mg; 250 mg; 500 mg; 750 mg; 1g, 1.5 g;7.5 g;125 mg/5 mL; 750 mg/50 mL

Urinary Tract Infection

Uncomplicated infections

  • Oral (tablets): 250 mg orally every 12 hours for 7 to 10 days
  • Parenteral: 750 mg IV or IM every 8 hour
  • Severe or complicated infections: 1.5 g IV or IM every 8 hours

Pneumonia

  • Uncomplicated infections: 750 mg IV or IM every 8 hours
  • Severe or complicated infections: 1.5 g IV or IM every 8 hours

Infectious Diseases Society of America (IDSA) and American Thoracic Society (ATS) Recommendations

  • 500 mg orally twice a day

Bacterial Infection

  • Oral (tablets): 250 or 500 mg orally every 12 hours
  • Parenteral: 750 mg to 1.5 g IV or IM every 8 hours
  • Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours may be needed

Bronchitis

  • Oral (tablets): 250 or 500 mg orally every 12 hours for 10 days
  • Parenteral: 750 mg to 1.5 g IV or IM every 8 hours

Skin and Structure Infection

  • Oral (tablets): 250 to 500 mg orally every 12 hours for 10 days
  • Parenteral: 750 mg IV or IM every 8 hours
  • Severe or complicated infections: 1.5 g IV or IM every 8 hours

Septicemia

  • Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours

Meningitis

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  • Life-threatening infections or infections due to less susceptible organisms: 1.5 g IV every 6 hours
  • Maximum dose: 3 g IV every 8 hours

Joint Infection

  • 1.5 g IV or IM every 8 hours

Osteomyelitis

  • 1.5 g IV or IM every 8 hours

Surgical Prophylaxis

Clean-contaminated or potentially contaminated surgical procedures

  • Preoperative: 1.5 g IV 30 to 60 minutes before the initial incision
  • Intraoperative (for prolonged procedures): 750 mg IV or IM every 8 hours
  • Open heart surgery: 1.5 g IV at induction of anesthesia and every 12 hours thereafter
  • Maximum dose: 6 g total

American Society of Health-System Pharmacists (ASHP), IDSA, Surgical Infection Society (SIS), and Society for Healthcare Epidemiology of America (SHEA) Recommendations

  • Preoperative dose: 1.5 g IV as a single dose
  • Redosing interval (from the start of preoperative dose): 4 hours

Pediatric Dose for Bacterial Infection

3 months to 12 years

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  • Oral suspension: 10 to 15 mg/kg orally twice a day
  • Maximum dose: 1 g/day
  • Tablets: 250 mg orally every 12 hours

13 years or older

  • Tablets: 250 or 500 mg orally every 12 hours

Parenteral

  • 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
  • Maximum dose: 1.5 g/dose

American Academy of Pediatrics (AAP) Recommendations

1 month or older

  • Mild to moderate infections: 20 to 30 mg/kg/day orally in 2 divided doses-
  • Maximum dose: 1 g/day

Parenteral

  • 7 days or younger: 50 mg/kg IV or IM every 12 hours

8 to 28 days

  • Up to 2 kg: 50 mg/kg IV or IM every 8 to 12 hours
  • Greater than 2 kg: 50 mg/kg IV or IM every 8 hours

1 month or older

  • Mild to moderate infections: 75 to 100 mg/kg/day IV or IM in 3 divided doses
  • Maximum dose: 4.5 g/day
  • Severe infections: 100 to 200 mg/kg/day IV or IM in 3 to 4 divided doses
  • Maximum dose: 6 g/day

Urinary Tract Infection

Oral (tablets)

  • 13 years or older: 250 mg orally every 12 hours for 7 to 10 days

Parenteral

  • 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
  • Maximum dose: 1.5 g/dose

Skin and Structure Infection

Oral (tablets)

  • 13 years or older: 250 or 500 mg orally every 12 hours for 10 days

Parenteral

  • 3 months or older: 50 to 100 mg/kg/day IV or IM in equally divided doses every 6 to 8 hours
  • Maximum dose: 1.5 g/dose

Side Effects of Cefuroxime

The most common

More common

Rare

Drug Interactions of Cefuroxime

Cefuroxime may interact with following drugs,supplements, & may change the efficacy of drugs

Pregnancy Catagory of Cefuroxime

FDA Pregnancy Category  B

Pregnancy

There are limited data from the use of cefuroxime in pregnant women. Studies in animals have shown no harmful effects on pregnancy, embryonal or foetal development, parturition or postnatal development. cefuroxime axetil should be prescribed to pregnant women only if the benefit outweighs the risk.

Lactation

This medication may  passes into breast milk. If you are a breast-feeding mother and are taking cefoperazone it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. It is not known if cefoperazone is safe for children under 6 months of age. There are no data on the effects of cefuroxime axetil on fertility in humans. Reproductive studies in animals have shown no effects on fertility.

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